Psychiatry related information on SC 27166

• In the rat, p.o. administration of loperamide and SC-27166 inhibited diarrhea at doses considerably lower than were necessary to produce withdrawal symptoms [1].

High impact information on SC 27166

• Nufenoxole is an orally active antidiarrhoeal agent which binds to opioid receptors in the brain and myenteric plexus of the intestine [2].
• Nufenoxole, a new antidiarrhoeal agent, inhibits fluid secretion in the human jejunum [2].
• After 0.2, 0.4, and 0.6 mg naloxone, pupillary constriction (0.618 to 0.540 cm, p less than 0.005) was measured in subjects receiving nufenoxole, whereas slight dilation (0.596 to 0.622 cm, p less than 0.05) was observed in those receiving loperamide [3].
• When administered orally loperamide and SC 27166 were devoid of opiate-like central nervous system activity [4].
• Morphine, loperamide and SC-27166 inhibited the contractions of electrically driven longitudinal muscle from guinea-pig ileum and naloxone antagonized these effects [1].

Biological context of SC 27166

• Single- and multiple-dose pharmacokinetics of nufenoxole in healthy human subjects [5].

Anatomical context of SC 27166

• In the anesthetized dog, i.v. administration of morphine and SC-27166 enhanced the contractile activity of circular muscle in proximal and distal duodenum and distal ileum but duodenal longitudinal muscle was relaxed; these effects were completely reversed by subsequent administration of naloxone [1].
• 6-keto PGF1 alpha and TXB2 synthesis by cultured colonic mucosa was also not affected by nufenoxole (50-800 ng/ml) [6].

Associations of SC 27166 with other chemical compounds

• Antidiarrheal and central nervous system activities of SC-27166 (2-[3 - 5 - methyl - 1, 3, 4 - oxadiazol - 2 - yl) - 3, 3 - diphenylpropyl] - 2 - azabicyclo [2.2.2]octane), a new antidiarrheal agent, resulting from binding to opiate receptor sites of brain and myenteric plexus [1].
• When compared with the reference standards morphine and diphenoxylate, these pharmacological studies indicated that SC-27166 has a high degree of separation of undesirable central nervous system actions from its antidiarrheal properties and may have important therapeutic potential [7].
• Metabolism and pharmacokinetics of nufenoxole in animals and humans: an example of stereospecific hydroxylation of an isoquinuclidine ring [8].

Analytical, diagnostic and therapeutic context of SC 27166

• Supportive pharmacological studies indicated that SC-27166 has equivocal analgesia in mice which is manifested at near toxic dose levels [7].
• SC-27166, which is chemically unrelated to opiates or neuroleptics, possesses potent constipating and antidiarrheal activity in several animal models [7].
• 1. Nufenoxole, a novel antidiarrhoeal agent, was well absorbed in rat, monkey and human after oral administration [8].

References